Search Results - "HEBEISEN, Paul" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

5‑(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

5‑(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

by Beaufils, Florent, Cmiljanovic, Natasa, Cmiljanovic, Vladimir, Bohnacker, Thomas, Melone, Anna, Marone, Romina, Jackson, Eileen, Zhang, Xuxiao, Sele, Alexander, Borsari, Chiara, Mestan, Jürgen, Hebeisen, Paul, Hillmann, Petra, Giese, Bernd, Zvelebil, Marketa, Fabbro, Doriano, Williams, Roger L, Rageot, Denise, Wymann, Matthias P
Published in Journal of medicinal chemistry (14.09.2017)

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6‑Alkoxy-5-aryl-3-pyridinecarboxamides, a New Series of Bioavailable Cannabinoid Receptor Type 1 (CB1) Antagonists Including Peripherally Selective Compounds

6‑Alkoxy-5-aryl-3-pyridinecarboxamides, a New Series of Bioavailable Cannabinoid Receptor Type 1 (CB1) Antagonists Including Peripherally Selective Compounds

by Röver, Stephan, Andjelkovic, Mirjana, Bénardeau, Agnès, Chaput, Evelyne, Guba, Wolfgang, Hebeisen, Paul, Mohr, Susanne, Nettekoven, Matthias, Obst, Ulrike, Richter, Wolfgang F, Ullmer, Christoph, Waldmeier, Pius, Wright, Matthew B
Published in Journal of medicinal chemistry (27.12.2013)

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In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci

In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci

by HEBEISEN, Paul, HEINZE-KRAUSS, Ingrid, ANGEHRN, Peter, HOHL, Peter, PAGE, Malcolm G. P, THEN, Rudolf L
Published in Antimicrobial Agents and Chemotherapy (01.03.2001)

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Enantioselective desymmetrizing palladium catalyzed carbonylation reactions: the catalytic asymmetric synthesis of quaternary carbon center containing 1,3-dienes

Enantioselective desymmetrizing palladium catalyzed carbonylation reactions: the catalytic asymmetric synthesis of quaternary carbon center containing 1,3-dienes

by Byrne, Simon J., Fletcher, Anthony J., Hebeisen, Paul, Willis, Michael C.
Published in Organic & biomolecular chemistry (01.01.2010)

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New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine

New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine

by Angehrn, Peter, Buchmann, Stefan, Funk, Christoph, Goetschi, Erwin, Gmuender, Hans, Hebeisen, Paul, Kostrewa, Dirk, Link, Helmut, Luebbers, Thomas, Masciadri, Raffaello, Nielsen, Joergen, Reindl, Peter, Ricklin, Fabienne, Schmitt-Hoffmann, Anne, Theil, Frank-Peter
Published in Journal of medicinal chemistry (11.03.2004)

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Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks

Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks

by Stojiljkovic, Uros, Meyer, Claudio, Boulay, Pierre, Hebeisen, Paul, Rageot, Denise, Wymann, Matthias P., Borsari, Chiara
Published in Synthesis (Stuttgart) (02.02.2023)

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Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-y1})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-y1})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

by Rageot, Denise, Bohnacker, Thomas, Melone, Anna, Langlois, Jean-Baptiste, Borsari, Chiara, Hillmann, Petra, Sele, Alexander M., Beaufils, Florent, Zvelebil, Marketa, Hebeisen, Paul, Loescher, Wolfgang, Burke, John, Fabbro, Doriano, Wymann, Matthias P.
Published in Journal of medicinal chemistry (22.11.2018)

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Abstract 293: Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitors suitable for the treatment of CNS disorders

Abstract 293: Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitors suitable for the treatment of CNS disorders

by Borsari, Chiara, Keles, Erhan, Treyer, Andrea, De Pascale, Martina, Hebeisen, Paul, Hamburger, Matthias, Wymann, Matthias P.
Published in Cancer research (Chicago, Ill.) (01.07.2021)

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Discovery and Preclinical Characterization of 5‑[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

Discovery and Preclinical Characterization of 5‑[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

by Rageot, Denise, Bohnacker, Thomas, Melone, Anna, Langlois, Jean-Baptiste, Borsari, Chiara, Hillmann, Petra, Sele, Alexander M, Beaufils, Florent, Zvelebil, Marketa, Hebeisen, Paul, Löscher, Wolfgang, Burke, John, Fabbro, Doriano, Wymann, Matthias P
Published in Journal of medicinal chemistry (21.11.2018)

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(S)‑4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase

(S)‑4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase

by Rageot, Denise, Bohnacker, Thomas, Keles, Erhan, McPhail, Jacob A, Hoffmann, Reece M, Melone, Anna, Borsari, Chiara, Sriramaratnam, Rohitha, Sele, Alexander M, Beaufils, Florent, Hebeisen, Paul, Fabbro, Doriano, Hillmann, Petra, Burke, John E, Wymann, Matthias P
Published in Journal of medicinal chemistry (11.07.2019)

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A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

by Borsari, Chiara, Rageot, Denise, Dall’Asen, Alix, Bohnacker, Thomas, Melone, Anna, Sele, Alexander M, Jackson, Eileen, Langlois, Jean-Baptiste, Beaufils, Florent, Hebeisen, Paul, Fabbro, Doriano, Hillmann, Petra, Wymann, Matthias P
Published in Journal of medicinal chemistry (26.09.2019)

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4‑(Difluoromethyl)-5-(4-((3R,5S)‑3,5-dimethylmorpholino)-6-((R)‑3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders

4‑(Difluoromethyl)-5-(4-((3R,5S)‑3,5-dimethylmorpholino)-6-((R)‑3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders

by Borsari, Chiara, Keles, Erhan, Rageot, Denise, Treyer, Andrea, Bohnacker, Thomas, Bissegger, Lukas, De Pascale, Martina, Melone, Anna, Sriramaratnam, Rohitha, Beaufils, Florent, Hamburger, Matthias, Hebeisen, Paul, Löscher, Wolfgang, Fabbro, Doriano, Hillmann, Petra, Wymann, Matthias P
Published in Journal of medicinal chemistry (25.11.2020)

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Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor

Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor

by De Pascale, Martina, Bissegger, Lukas, Tarantelli, Chiara, Beaufils, Florent, Prescimone, Alessandro, Mohamed Seid Hedad, Hayget, Kayali, Omar, Orbegozo, Clara, Raguž, Luka, Schaefer, Thorsten, Hebeisen, Paul, Bertoni, Francesco, Wymann, Matthias P., Borsari, Chiara
Published in European journal of medicinal chemistry (15.02.2023)

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Scalable, Economical, and Practical Synthesis of 4‑(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors

Scalable, Economical, and Practical Synthesis of 4‑(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors

by Rageot, Denise, Beaufils, Florent, Borsari, Chiara, Dall’Asen, Alix, Neuburger, Markus, Hebeisen, Paul, Wymann, Matthias P
Published in Organic process research & development (15.11.2019)

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Abstract 665: Discovery and preclinical characterization of PQR626: A potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of tuberous sclerosis complex

Abstract 665: Discovery and preclinical characterization of PQR626: A potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of tuberous sclerosis complex

by Borsari, Chiara, Keles, Erhan, Rageot, Denise, Melone, Anna, Bohnacker, Thomas, Batchelor, Lucinda Kate, De Pascale, Martina, Hebeisen, Paul, Hillmann, Petra, Fabbro, Doriano, Wymann, Matthias
Published in Cancer research (Chicago, Ill.) (15.08.2020)

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5-HT2C receptor agonists for the treatment of obesity. Biological and chemical adventures

5-HT2C receptor agonists for the treatment of obesity. Biological and chemical adventures

by Adams, D, Benardeau, A, Bickerdike, MJ, Bentley, JM, Bissantz, C, Bourson, A, Cliffe, IA, Hebeisen, P, Kennett, GA, Knight, AR, Malcolm, CS, Mizrahi, J, Plancher, JM, Richter, H, Rover, S, Taylor, S, Vickers, SP
Published in Chimia (01.09.2004)

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Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability

Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability

by Borsari, Chiara, Keles, Erhan, Treyer, Andrea, De Pascale, Martina, Hebeisen, Paul, Hamburger, Matthias, Wymann, Matthias P
Published in MedChemComm (28.04.2021)

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Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl–Pyrimidine Moiety

Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl–Pyrimidine Moiety

by Borsari, Chiara, Rageot, Denise, Beaufils, Florent, Bohnacker, Thomas, Keles, Erhan, Buslov, Ivan, Melone, Anna, Sele, Alexander M, Hebeisen, Paul, Fabbro, Doriano, Hillmann, Petra, Wymann, Matthias P
Published in ACS medicinal chemistry letters (10.10.2019)

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Ring opening of cyclic sulfamidates with bromophenyl metal reagents: complementarity of sulfamidates and aziridines

Ring opening of cyclic sulfamidates with bromophenyl metal reagents: complementarity of sulfamidates and aziridines

by Hebeisen, Paul, Weiss, Urs, Alker, André, Staempfli, Andreas
Published in Tetrahedron letters (12.10.2011)

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Molecular Structure and Crystal Packing of Monofluoromethoxyarenes

Molecular Structure and Crystal Packing of Monofluoromethoxyarenes

by Hebeisen, Paul, Weiss, Urs, Alker, André, Kuhn, Bernd, Müller, Klaus, Wang, Fang, Surya Prakash, G. K.
Published in European journal of organic chemistry (01.08.2018)

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